Description
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 (Edwards and Wandless 2007). Rapamycin is an autophagy activator, an immunosuppressant (Rangaraju et al. 2010).
MOA
MTOR inhibitor
ITP
Drug Targets
FGF2
FKBP1A
MTOR (drug-ligand rendering)
Reactome Pathway
R-HSA-449147:Signaling by Interleukins
R-HSA-5663202:Diseases of signal transduction by growth factor receptors and second messengers
R-HSA-9006925:Intracellular signaling by second messengers
R-HSA-1257604:PIP3 activates AKT signaling
R-HSA-3700989:Transcriptional Regulation by TP53
R-HSA-6785807:Interleukin-4 and Interleukin-13 signaling
R-HSA-5633007:Regulation of TP53 Activity
R-HSA-9612973:Autophagy
R-HSA-1632852:Macroautophagy
R-HSA-6807070:PTEN Regulation
References
Edwards, Sarah R., and Thomas J. Wandless. 2007. “The Rapamycin-Binding Domain of the Protein Kinase Mammalian Target of Rapamycin Is a Destabilizing Domain.” Journal of Biological Chemistry 282 (18): 13395–401. https://doi.org/10.1074/jbc.m700498200.
Rangaraju, Sunitha, Jonathan D. Verrier, Irina Madorsky, Jessica Nicks, William A. Dunn, and Lucia Notterpek. 2010. “Rapamycin Activates Autophagy and Improves Myelination in Explant Cultures from Neuropathic Mice.” The Journal of Neuroscience 30 (34): 11388–97. https://doi.org/10.1523/jneurosci.1356-10.2010.